VAP 20 concentrate 20 µg/ml 1 ml, 10 pcs.

Proteaglandin E₁ drug. It improves microcirculation and peripheral circulation, has angioprotective effect. When administered systemically it causes relaxation of smooth muscle fibers, has a vasodilator effect, decreases ARF, lowers BP.

In this case there is a reflex increase of cardiac output and HR. It improves rheological properties of blood by increasing the elasticity of erythrocytes and reducing platelet aggregation and neutrophil activity, increases blood fibrinolytic activity.

It affects the metabolism, increases the utilization of glucose and oxygen, inhibits the release of free radicals and lysosomal enzymes from granulocytes and macrophages, stimulates protein synthesis, has a beneficial effect on lipid metabolism (inhibiting cholesterol synthesis and reducing LDL concentration), inhibits proliferation of smooth muscle cells.

It has a stimulating effect on the smooth muscles of the intestine, bladder and uterus; it suppresses the secretion of gastric juice.

In intracavernosal administration blocks α₁-adrenoreceptors in penile tissues and causes relaxation effect on smooth muscle of corpora cavernosa, increases blood flow and improves microcirculation.

Dilation of cavernous arteries and vessels of trabecular smooth muscles of cavernous bodies leads to rapid increase of blood inflow and dilatation of lacunar spaces in cavernous bodies. Venous outflow through the vessels located under the proteinous shell is restricted, which stimulates the development of an erection (“corporal veno-occlusive mechanism”). The onset of action is 5-10 minutes, the duration is 1-3 hours.

Indications

The need for temporary maintenance of the arterial ductus function until corrective surgery in congenital ductus-dependent heart defects in newborns (including mitral atresia, pulmonary atresia, tricuspid valve atresia, Fallo’s tetrad).

Chronic obliterating arterial diseases of stage III-IV (according to Fontaine classification). Obliterating endarteritis with severe intermittent claudication (when surgical revascularization of the lower extremity is impossible), obliterating atherosclerosis, diabetic angiopathy, obliterating thrombangiitis (Buerger’s disease), Raynaud’s syndrome with trophic disorders, vasculitis, scleroderma, calf cramps, damaging effects of physical factors, especially ultra-limited vibration.

The treatment of erectile dysfunction of neurogenic, vascular, psychogenic or mixed etiology; conducting pharmacological test in the complex of diagnostic tests in erectile dysfunction.

Active ingredient

Interaction

Directions for use

Special Instructions

Caution is used by/a and intravenously in acute and subacute myocardial infarction, myocardial infarction within the last 6 months, severe or unstable angina pectoris, decompensated chronic heart failure, arterial hypotension, cardiovascular insufficiency, pulmonary edema, severe arrhythmias, bronchoobstructive syndrome (severe with signs of respiratory failure), infiltrative changes in lungs, hepatic insufficiency (incl.liver failure (including anamnesis), at high risk of bleeding (including in patients with gastric or duodenal ulcer disease, severe lesions of cerebral vessels, proliferative retinopathy with propensity to bleeding, extensive trauma), hemodialysis, type 1 diabetes, especially in extensive vascular lesions (in elderly patients); during the use of vasodilators or anticoagulants; in newborns (risk of bradypnea, hypotension, tachycardia or hyperthermia).

Cautiously administer intracavernosal in thrombocytopenia, polycythemia, thrombophlebitis, venous thrombosis (including if predisposed), hyperviscosity, balanitis, urethritis.

Do not use in patients with a tendency to addiction and/or mental or intellectual disabilities.

In case of clotting disorders or concomitant therapy with drugs that affect the clotting system, clotting parameters should be monitored regularly during treatment with alprostadil. During systemic administration it is necessary to monitor the parameters of central hemodynamics and biochemical blood parameters.

Long-term continuous administration may cause apnea, negative effect on the structure of the arterial duct wall with increased risk of rupture, thinning of the muscular layer of the pulmonary artery. With treatment duration of more than 4 weeks, reversible cortical proliferation of tubular bones is possible.

In newborns it should be used under constant BP control, with mandatory conditions for ventilation.

There is currently no experience with intracavernous administration in patients younger than 18 years and older than 75 years.

Alprostadil is not intended for concomitant use with other drugs for the treatment of erectile dysfunction.

The dosage form of alprostadil used must be closely matched to the specific indication for its use.

Features

Alprostadil is rapidly metabolized when administered intravenously. During a single passage through the lungs it is metabolized up to 60-90%. Enzymatic oxidation produces 3 biologically active metabolites: 15-keto-PGE1, 15-keto-13,14-dihydro-PGE1 and 13,14-dihydro-PGE1. The keto metabolites have a lower biological effect than alprostadil; the 13,14-dihydro-PGE1 metabolite has comparable action to PGE1. The pharmacodynamic effect is mainly due to this biologically active metabolite. The T1/2 13,14-dihydro-PGE1 is about 1 min. The major metabolites are excreted mainly in the urine and, to a lesser extent, in the feces.

In intracavernous administration, the concentration of alprostadil and its major metabolite, 15-oxo-13,14-dihydro-PgE1, is determined only in the cavernous bodies. After intracavernous injection of 20 µg of alprostadil, the content of the main metabolite in the peripheral bloodstream increased and peaked 30 min after injection and then returned to baseline levels 60 min after injection, while the levels of alprostadil in the peripheral bloodstream were slightly higher than baseline. Alprostadil is metabolized very rapidly upon entering the large circulatory circuit during intracavernous injection. It is excreted as metabolites.

Contraindications

Chronic heart failure, pulmonary edema, cardiac rhythm disturbances, myocardial infarction within the last 6 months; lung infiltrative changes, bronchial asthma; liver function disorders, liver diseases (including anamnesis); gastrointestinal ulcers in anamnesis; hypersensitivity to alprostadil; pregnancy, lactation.

For intracavernous administration: diseases predisposing to priapism (sickle cell anemia, myeloma disease, leukemia); anatomical deformities of the penis (angulation, cavernous fibrosis, Peyronie’s disease). Do not use in patients with a penile implant, as well as with contraindications for sexual intercourse.

Side effects

Digestive system disorders: diarrhea, nausea, vomiting, increased transaminase activity; rarely – hyperbilirubinemia, peritoneal symptoms.

Cardiovascular system: arterial hypotension, tachycardia, pain in the heart region; rarely – heart failure, heart rhythm disorders, AV-blockade, acute pulmonary edema.

CNS and peripheral nervous system disorders: headache, psychosis, convulsions of central genesis, paresthesia; rarely – lethargy.

Respiratory system disorders: rarely – tachypnea, respiratory distress syndrome.

Hematopoietic and coagulation system disorders: leukocytosis, leukopenia; rarely – bleeding, hypochromic anemia, thrombocytopenia.

Urinary system: rarely – anuria, renal failure, hematuria.

Mechanisms: rarely – hypoglycemia, hypercapnia.

Muscular system disorders: joint pain, neck muscle tension, reversible hyperostosis of tubular bones.

Allergic reactions: skin rash, itching.

Others: hyperthermia, redness of the skin, increased sweating, swelling of the limb in which the infusion is administered may occur.

In intracavernous injection, pain in the penis, prolonged erection and priapism are possible; rare – fibrosis, swelling, fever, numbness, rashes on the penis, balanitis, hemorrhages, itching and swelling of the injection site, urethral bleeding, fungal infection, phimosis, painful erections and ejaculation disorders, pain in the testicles, testicular swelling, pain and tension in the scrotum, increased frequency of urination, urinary incontinence, pain in the buttocks, legs, abdomen, pain in the pelvis, lower back, flu-like syndrome, hypoesthesia, myasthenia.

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